阿貝卡爾

**阿貝卡爾**
臨床資料
ATC碼	未分配;
藥物動力學數據
生物半衰期	3.4 hours (IV), 7 hours (oral)
識別資訊
	IUPAC命名法 propan-2-yl 4-(methoxymethyl)-6-(phenylmethoxy) -9H-pyrido[5,4-b]indole-3-carboxylate; ;
CAS號	111841-85-1
PubChem CID	65914;
ChemSpider	59323 ;
UNII	IZM1PNJ3JL;
KEGG	D02594 ;
ChEMBL	ChEMBL454095 ;
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID40149745 ;
化學資訊
化學式	C24H24N2O4
摩爾質量	404.47 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	SMILES COCc3c(C(=O)OC(C)C)ncc4[nH]c2ccc(OCc1ccccc1)cc2c34;
	InChI InChI=1S/C24H24N2O4/c1-15(2)30-24(27)23-19(14-28-3)22-18-11-17(29-13-16-7-5-4-6-8-16)9-10-20(18)26-21(22)12-25-23/h4-12,15,26H,13-14H2,1-3H3 ; Key:RLFKILXOLJVUNF-UHFFFAOYSA-N ;

阿貝卡爾（英語：Abecarnil，代號：ZK-112,119）是一種來自β-咔啉家族的抗焦慮藥。它是相對較新開發的一類藥物之一，稱為非苯二氮䓬類藥物，與較早的苯二氮䓬類藥物具有相似的作用，但化學結構截然不同。它是一種部分激動劑，選擇性地作用於GABA_A受體的苯二氮䓬位點。^[1]

阿貝卡爾最初是作為抗焦慮藥物開發的，但尚未商業化開發用於人類，目前主要用於研究開發其他新型鎮靜和抗焦慮藥物。對其作用的調查仍在繼續，它看起來很可能被開發用於治療焦慮症，^[2]以及作為一種不太容易上癮的替代藥物來治療苯二氮䓬類藥物^[3]和酒精^[4]成癮。與非選擇性全激動劑苯二氮䓬類藥物相比，阿貝卡尼的耐受性和戒斷問題也可能更少。^[5]

阿貝卡爾是一種相對亞型選擇性的藥物，主要產生抗焦慮作用，具有相對較弱的鎮靜或肌肉鬆弛作用，^[6]^[7]並且不會顯着增強酒精的作用。^[8]

阿貝卡爾的濫用可能性被認為低於苯二氮卓類藥物，^[9]突然停止治療後僅會出現輕微的戒斷症狀。^[10]

參見[編輯]

參考資料[編輯]

^ Ozawa, M; Nakada, Y; Sugimachi, K; Yabuuchi, F; Akai, T; Mizuta, E; Kuno, S; Yamaguchi, M. Pharmacological characterization of the novel anxiolytic beta-carboline abecarnil in rodents and primates. Japanese Journal of Pharmacology. Mar 1994, 64 (3): 179–87. PMID 7912751. doi:10.1254/jjp.64.179 .
^ Aufdembrinke B. Abecarnil, a new beta-carboline, in the treatment of anxiety disorders. British Journal of Psychiatry. 1998, 34 (34): 55–63. PMID 9829018. S2CID 24311570. doi:10.1192/S0007125000293537.
^ Pinna G, Galici R, Schneider HH, Stephens DN, Turski L. Alprazolam dependence prevented by substituting with the beta-carboline abecarnil. Proceedings of the National Academy of Sciences of the United States of America. Mar 1997, 94 (6): 2719–23. Bibcode:1997PNAS...94.2719P. PMC 20156 . PMID 9122263. doi:10.1073/pnas.94.6.2719 .
^ Jung ME, Wallis CJ, Gatch MB, Lal H. Abecarnil and alprazolam reverse anxiety-like behaviors induced by ethanol withdrawal. Alcohol. Jun 2000, 21 (2): 161–8. PMID 10963939. doi:10.1016/S0741-8329(00)00079-3.
^ Löscher W, Hönack D. Withdrawal precipitation by benzodiazepine receptor antagonists in dogs chronically treated with diazepam or the novel anxiolytic and anticonvulsant beta-carboline abecarnil. Naunyn Schmiedebergs Arch. Pharmacol. April 1992, 345 (4): 452–60. PMID 1352384. S2CID 20486955. doi:10.1007/BF00176624.
^ Krause W, Schutt B, Duka T. Pharmacokinetics and acute toleration of the beta-carboline derivative abecarnil in man. Arzneimittelforschung. May 1990, 40 (5): 529–32. PMID 1974428.
^ Duka T, Schutt B, Krause W, Dorow R, McDonald S, Fichte K. Human studies on abecarnil, a new beta-carboline anxiolytic: safety, tolerability and preliminary pharmacological profile. British Journal of Clinical Pharmacology. Apr 1993, 35 (4): 386–94. PMC 1381549 . PMID 8097921. doi:10.1111/j.1365-2125.1993.tb04155.x.
^ Stephens DN, Schneider HH, Kehr W, Andrews JS, Rettig KJ, Turski L, Schmiechen R, Turner JD, Jensen LH, et al. Abecarnil, a metabolically stable, anxioselective beta-carboline acting at benzodiazepine receptors. Journal of Pharmacology and Experimental Therapeutics. Apr 1990, 253 (1): 334–43. PMID 1970361.
^ Sannerud CA, Ator NA, Griffiths RR. Behavioral pharmacology of abecarnil in baboons: self-injection, drug discrimination and physical dependence. Behavioural Pharmacology. Oct 1992, 3 (5): 507–516. PMID 11224153. S2CID 32081258. doi:10.1097/00008877-199210000-00009.
^ Ballenger JC, McDonald S, Noyes R, Rickels K, Sussman N, Woods S, Patin J, Singer J. The first double-blind, placebo-controlled trial of a partial benzodiazepine agonist abecarnil (ZK 112-119) in generalized anxiety disorder. Psychopharmacology Bulletin. 1991, 27 (2): 171–9. PMID 1681563.

[1] Ozawa, M; Nakada, Y; Sugimachi, K; Yabuuchi, F; Akai, T; Mizuta, E; Kuno, S; Yamaguchi, M. Pharmacological characterization of the novel anxiolytic beta-carboline abecarnil in rodents and primates. Japanese Journal of Pharmacology. Mar 1994, 64 (3): 179–87. PMID 7912751. doi:10.1254/jjp.64.179 .

[2] Aufdembrinke B. Abecarnil, a new beta-carboline, in the treatment of anxiety disorders. British Journal of Psychiatry. 1998, 34 (34): 55–63. PMID 9829018. S2CID 24311570. doi:10.1192/S0007125000293537.

[3] Pinna G, Galici R, Schneider HH, Stephens DN, Turski L. Alprazolam dependence prevented by substituting with the beta-carboline abecarnil. Proceedings of the National Academy of Sciences of the United States of America. Mar 1997, 94 (6): 2719–23. Bibcode:1997PNAS...94.2719P. PMC 20156 . PMID 9122263. doi:10.1073/pnas.94.6.2719 .

[4] Jung ME, Wallis CJ, Gatch MB, Lal H. Abecarnil and alprazolam reverse anxiety-like behaviors induced by ethanol withdrawal. Alcohol. Jun 2000, 21 (2): 161–8. PMID 10963939. doi:10.1016/S0741-8329(00)00079-3.

[5] Löscher W, Hönack D. Withdrawal precipitation by benzodiazepine receptor antagonists in dogs chronically treated with diazepam or the novel anxiolytic and anticonvulsant beta-carboline abecarnil. Naunyn Schmiedebergs Arch. Pharmacol. April 1992, 345 (4): 452–60. PMID 1352384. S2CID 20486955. doi:10.1007/BF00176624.

[6] Krause W, Schutt B, Duka T. Pharmacokinetics and acute toleration of the beta-carboline derivative abecarnil in man. Arzneimittelforschung. May 1990, 40 (5): 529–32. PMID 1974428.

[7] Duka T, Schutt B, Krause W, Dorow R, McDonald S, Fichte K. Human studies on abecarnil, a new beta-carboline anxiolytic: safety, tolerability and preliminary pharmacological profile. British Journal of Clinical Pharmacology. Apr 1993, 35 (4): 386–94. PMC 1381549 . PMID 8097921. doi:10.1111/j.1365-2125.1993.tb04155.x.

[8] Stephens DN, Schneider HH, Kehr W, Andrews JS, Rettig KJ, Turski L, Schmiechen R, Turner JD, Jensen LH, et al. Abecarnil, a metabolically stable, anxioselective beta-carboline acting at benzodiazepine receptors. Journal of Pharmacology and Experimental Therapeutics. Apr 1990, 253 (1): 334–43. PMID 1970361.

[9] Sannerud CA, Ator NA, Griffiths RR. Behavioral pharmacology of abecarnil in baboons: self-injection, drug discrimination and physical dependence. Behavioural Pharmacology. Oct 1992, 3 (5): 507–516. PMID 11224153. S2CID 32081258. doi:10.1097/00008877-199210000-00009.

[10] Ballenger JC, McDonald S, Noyes R, Rickels K, Sussman N, Woods S, Patin J, Singer J. The first double-blind, placebo-controlled trial of a partial benzodiazepine agonist abecarnil (ZK 112-119) in generalized anxiety disorder. Psychopharmacology Bulletin. 1991, 27 (2): 171–9. PMID 1681563.

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